期刊论文

中文

中南药学

1672-2981

2010

8

10

751-753

10.3969/j.issn.1672-2981.2010.10.010

基金项目：湖南省教育厅项目（07C474）.

本校为第一机构

目的研究合成喹诺酮类抗菌药物加替沙星的方法。方法以2,4,5-三氟-3-甲氧基苯甲酸为起始原料,经酰氯化、缩合、水解脱羧后与原甲酸三乙酯缩合、烯胺化、环合,然后与硼酸螯合,再与2-甲基哌嗪缩合后水解得到加替沙星。结果加替沙星总收率43.2%。结论该工艺操作简单,收率高,适合工业化大生产的要求。

Objective To synthesize gatifloxacin as an antibiotic agent.Methods Gatifloxacin was synthesized from 3-methoxy-2,4,5-trifluorobenzoic acid by acylchorination,condensed with diethyl malonate,partial hydrolysis and decarboxylation,condensed with triethylorthoformate,cyclopropylamine displacement,cyclization,reacted with triacyloxyborate,and condensed with 2-methylpiperazine and then hydrosis.Results The total yield of gatifloxacin was 43.2%.Conclusion The process with a high ...